Name: Prostaglandin E2 (PGE2)
Brand: Selleck Chemicals
SKU: S3003
Rating: 5 (29 reviews)

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Batch: Zuiverheid: >97%

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
Datasheet
SDS

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
Datasheet
SDS

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
NMR
Datasheet
SDS

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
NMR
Datasheet
SDS

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
NMR
Datasheet
SDS

97

Gerelateerde doelwitten	Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR
Overige PGES Inhibitoren	Yakuchinone A

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
HeLa	Function assay			TP_TRANSPORTER: uptake in PGT-expressing HeLa cells, Km = 0.094 μM.	7754369
HeLa	Function assay			TP_TRANSPORTER: uptake in PGT-expressing HeLa cells, K1/2 = 0.1 μM.	8787677
S2	Function assay			TP_TRANSPORTER: uptake in OCT2-expressing S2 cells, Km = 0.0289 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OAT4-expressing S2 cells, Km = 0.154 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OAT3-expressing S2 cells, Km = 0.345 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OCT1-expressing S2 cells, Km = 0.657 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OAT2-expressing S2 cells, Km = 0.713 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OAT1-expressing S2 cells, Km = 0.97 μM.	11907186
HEK293	Function assay			Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cells, IC50 = 0.0007 μM.	12643927
HEK293	Function assay			EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptor, EC50 = 0.003 μM.	12643927
Sf9	Function assay			TP_TRANSPORTER: uptake (vesicle) in membrane vesicles from MRP4-expressing Sf9 cells, Km = 3.4 μM.	12835412
HEK293	Function assay			Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells, Ki = 0.00033 μM.	17531488
HEK293	Function assay			Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells, Ki = 0.00079 μM.	17531488
HEK293	Function assay			Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells, Ki = 0.0049 μM.	17531488
HEK293	Function assay			Displacement of [3H]PGE2 from human EP1 receptor expressed in HEK293 cells, Ki = 0.0091 μM.	17531488
HEK293	Function assay			Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release, EC50 = 0.0002 μM.	19250823
HEK293	Function assay			Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release, EC50 = 0.0007 μM.	19250823
HEK293	Function assay			Inhibition of rat EP4 receptor expressed in HEK293 cells, IC50 = 0.0021 μM.	19250823
HEK293	Function assay			Inhibition of rat EP2 receptor expressed in HEK293 cells, IC50 = 0.0052 μM.	19250823
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.0031 μM.	22119471
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.005 μM.	22119471
CHO	Function assay		20 mins	Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting, Ki = 0.006 μM.	22119471
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.022 μM.	22119471
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.0031 μM.	22386979
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.005 μM.	22386979
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.006 μM.	22386979
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.022 μM.	22386979
CHEM1	Function assay		2 hrs	Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs, Ki = 0.00045 μM.	23403082
CHEM1	Function assay		2 hrs	Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs, IC50 = 0.0011 μM.	23403082
CHO	Function assay	100 nM		Activity at recombinant EP1 receptor (unknown origin) expressed in CHO cells co-expressing Gq protein at 100 nM by electrical cell substrate impedance sensing system	25701254
CHO	Function assay	100 nM		Activity at recombinant EP4 receptor (unknown origin) expressed in CHO cells co-expressing Gs protein at 100 nM by electrical cell substrate impedance sensing system	25701254
CHO	Function assay	100 nM		Activity at recombinant EP3 receptor (unknown origin) expressed in CHO cells co-expressing Gi protein at 100 nM by electrical cell substrate impedance sensing system	25701254
CHO	Function assay		30 mins	Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.0019 μM.	26985320
CHO	Function assay			Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.0025 μM.	26985320
CHO	Function assay			Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.0037 μM.	26985320
CHO	Function assay		30 mins	Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.0075 μM.	26985320
Chem1	Function assay			Agonist activity at human FP receptor expressed in human Chem1 cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.25 μM.	26985320
HEK293	Function assay		90 mins	Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay, EC50 = 0.346 μM.	26985320
CHO	Function assay		30 mins	Agonist activity at human IP receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.347 μM.	26985320
HEK293	Function assay			Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells, IC50 = 0.0026 μM.	26988801
HEK293	Function assay		120 mins	Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method, IC50 = 0.00055 μM.	27876250
HEK293	Function assay		120 mins	Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method, IC50 = 0.0026 μM.	27876250
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Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	352.47	Formule	C₂₀H₃₂O₅	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	363-24-6	SDF downloaden		Opslag van stamoplossingen	Oplossingen zijn onstabiel. Bereid vers of koop kleine, voorverpakte formaten. Herverpakken na ontvangst.
Synoniemen	Dinoprostone			Smiles	CCCCCC(C=CC1C(CC(=O)C1CC=CCCCC(=O)O)O)O

Oplosbaarheid

In vitro
Batch:

DMSO : 70 mg/mL (198.59 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 70 mg/mL

Water : 2.5 mg/mL

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	3.500mg/ml (9.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 70 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

In vitro	PGE2 werkt via EP4-receptoren op osteoclasten tijdens de progressie van OA en OA-gerelateerde pijn.
In vivo	PGE2 (0,3 μg/kg, i.p.) vermindert significant het aantal peritoneale macrofagen dat fagocytose van de methacrylaatmicrobolletjes ondergaat bij ratten.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/6804558/

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT06129604	Recruiting	Colorectal Carcinoma (CRC)\|Endometrial Carcinoma (EC)	University of Oklahoma	April 3 2024	Phase 2
NCT06307678	Completed	Periapical; Infection	Ataturk University	July 7 2023	Not Applicable
NCT06190132	Completed	Uremic Pruritus in Hemodialysis Patients	Ain Shams University	April 1 2023	Not Applicable

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Prostaglandin E2 (PGE2) Prostaglandin Receptor-agonist

Chemische structuur

Moleculair gewicht: 352.47